XB-ART-34830
Bioorg Med Chem Lett
2006 Oct 01;1619:5244-8. doi: 10.1016/j.bmcl.2006.05.031.
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Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers.
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Morpholin-2-one-5-carboxamide derivatives were prepared by using the one-pot Ugi multicomponent reaction and evaluated for blocking effects on T- and N-type Ca(2+) channels. Among them, compound 5i produced the highest potency (IC(50)=0.45+/-0.02 microM), while compounds 5d, 5f, 5k, 5n, 5o, and 6m produced relatively high potency as well as selectivity on T-type Ca(2+) channels. These novel scaffolds showed potent and selective T-type Ca(2+) channel blocking activities.
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